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[N-(2-氧代-3,5,7-环庚三烯-1-基)]氨基氧代乙酸乙酯(AY-25,674)对环3',5'-核苷酸形成及磷酸二酯酶活性的影响。

Effects of [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) on cyclic 3',5'-nucleotide formation and phosphodiesterase activity.

作者信息

Pugsley T A, Lippmann W

出版信息

Experientia. 1979 Jan 15;35(1):88-90. doi: 10.1007/BF01917895.

Abstract

The orally-effective antiallergic compound [N-(2-oxo-3,5,7-cycloheptatrien-1-yl)] aminooxoacetic acid ethyl ester (AY-25,674) exhibited a potency equivalent to or 3 times less than theophylline in inhibiting guinea-pig lung and beef heart PDE, respectively, AY-25,674 did not affect the basal activity of guinea-pig lung adenyl cyclase. Although part of the antiallergic activity of AY-25,674 may be due to the ability to elevate cyclic AMP levels by PDE inhibition, other modes of action appear to be of greater relevance.

摘要

口服有效的抗过敏化合物[N-(2-氧代-3,5,7-环庚三烯-1-基)]氨基氧乙酸乙酯(AY-25,674)在抑制豚鼠肺和牛心磷酸二酯酶(PDE)方面,其效力分别相当于茶碱或比茶碱低3倍。AY-25,674不影响豚鼠肺腺苷酸环化酶的基础活性。虽然AY-25,674的部分抗过敏活性可能归因于通过抑制磷酸二酯酶来提高环磷酸腺苷水平的能力,但其他作用方式似乎更具相关性。

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